1rtl
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| , resolution 2.75Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | H STRAIN (Hepatitis C virus) | ||||||
| Related: | 1N1L
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR
OverviewOverview
[reaction: see text] In this, the first of two Letters, we describe how a P3/P4 urea linking unit was used to greatly enhance the biochemical and replicon potency of inhibitors based upon the pyrrolidine-5,5-trans-lactam template. Compound 7b demonstrated a 100 nM IC(50) in the replicon cell-based surrogate HCV assay.
About this StructureAbout this Structure
1RTL is a Protein complex structure of sequences from Hepatitis c virus. Full crystallographic information is available from OCA.
ReferenceReference
Pyrrolidine-5,5-trans-lactams. 4. Incorporation of a P3/P4 urea leads to potent intracellular inhibitors of hepatitis C virus NS3/4A protease., Slater MJ, Amphlett EM, Andrews DM, Bamborough P, Carey SJ, Johnson MR, Jones PS, Mills G, Parry NR, Somers DO, Stewart AJ, Skarzynski T, Org Lett. 2003 Nov 27;5(24):4627-30. PMID:14627400
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